2346-26-1Relevant articles and documents
Discovery, synthesis, and evaluation of N-substituted amino-2(5H)- oxazolones as novel insecticides activating nicotinic acetylcholine receptors
Zhang, Wenming,Barry, James D.,Cordova, Daniel,McCann, Stephen F.,Benner, Eric A.,Hughes, Kenneth A.
, p. 2188 - 2192 (2014)
N-Substituted amino-2(5H)-oxazolones A are a novel class of insecticides acting as nicotinic acetylcholine receptor (nAChR) agonists and show potent activity against hemipteran insect species. Here we report the discovery and preparation of this class of chemistry. Our efforts in SAR elucidation, biological activity evaluation, as well as mode-of-action studies are also presented.
MODIFIED COMPOUND OF ANDROGRAPHOLIDE
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Paragraph 0557-0559, (2019/01/04)
The present disclosure discloses a modified compound of andrographolide, and particularly discloses a compound shown in formula (I) and (II) or a pharmaceutically acceptable salt thereof.
Structure Property Relationships of Carboxylic Acid Isosteres
Lassalas, Pierrik,Gay, Bryant,Lasfargeas, Caroline,James, Michael J.,Tran, Van,Vijayendran, Krishna G.,Brunden, Kurt R.,Kozlowski, Marisa C.,Thomas, Craig J.,Smith, Amos B.,Huryn, Donna M.,Ballatore, Carlo
, p. 3183 - 3203 (2016/05/19)
The replacement of a carboxylic acid with a surrogate structure, or (bio)-isostere, is a classical strategy in medicinal chemistry. The general underlying principle is that by maintaining the features of the carboxylic acid critical for biological activity, but appropriately modifying the physicochemical properties, improved analogs may result. In this context, a systematic assessment of the physicochemical properties of carboxylic acid isosteres would be desirable to enable more informed decisions of potential replacements to be used for analog design. Herein we report the structure-property relationships (SPR) of 35 phenylpropionic acid derivatives, in which the carboxylic acid moiety is replaced with a series of known isosteres. The data set generated provides an assessment of the relative impact on the physicochemical properties that these replacements may have compared to the carboxylic acid analog. As such, this study presents a framework for how to rationally apply isosteric replacements of the carboxylic acid functional group.
OXAZOLO[5,4-C]QUINOLIN-2-ONE COMPOUNDS AS BROMODOMAIN INHIBITORS
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Paragraph 00227, (2014/10/04)
The present invention relates to compounds useful as bromodomain inhibitors. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compounds and compositions in the treatment of various diseases and disorders.
Dihydroindolone compounds, a process for their preparation and pharmaceutical compositions containing them
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Page/Page column 9, (2011/02/26)
Compounds of formula (I): wherein: m and n represent 1 or 2,A represents a pyrrolyl group,X represents a C(O), S(O) or SO2 group,R1 and R2 represent an alkyl group or, together with the nitrogen atom carrying them, form a heterocyclic group,R3 and R4, together with the atoms carrying them, form a heterocyclic group,R5 represents a hydrogen atom or an alkyl group,R6 represents a hydrogen atom or a halogen atom. Medicinal products containing the same which are useful in treating cancer.
New heterocyclic inputs for the povarov multicomponent reaction
Vicente-Garcia, Esther,Ramon, Rosario,Lavilla, Rodolfo
supporting information; experimental part, p. 2237 - 2246 (2011/09/15)
Oxa-, thia- and imidazolones are reactive inputs as electron-rich olefin components in Povarov reactions. On interaction with anilines and aldehydes, these substrates afford the corresponding multicomponent adducts in a regioselective manner. Intramolecular processes are also explored. Post-condensation oxidation provides convenient access to a variety of fused quinoline derivatives. Georg Thieme Verlag Stuttgart ? New York.
ARYLOXYALKYLCARBAMATE-TYPE DERIVATIVES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS
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Page/Page column 6, (2008/06/13)
The invention relates to a compound of formula (I): [image] Wherein m, n, X, Y, R1, R2, R3 and R4 are as defined herein. The invention also relates to the use of same in therapeutics.
INDOLES HAVING ANTI-DIABETIC ACTIVITY
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Page/Page column 41, (2008/06/13)
Indoles of Formula (I) having -X-aryl-(CH2)x#191-oxazolidinedione and -X-heteroaryl-(CH2)X-oxazolidinedione substituents on the N atom of the indole ring, where x is 0 or 1, and -X-is a bond or -CH2-, and their thiazolidinedione analogs, are PPAR gamma agonists or partial agonists and are useful in the treatment and control of type II diabetes, including hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
Electrolytic partial fluorination of organic compounds. Part 78: Regioselective anodic fluorination of 2-oxazolidinones
Cao, Yi,Suzuki, Katsutoshi,Tajima, Toshiki,Fuchigami, Toshio
, p. 6854 - 6859 (2007/10/03)
Various 2-oxazolidinones were galvanostatically electrooxidized in the presence of various fluoride salts. It was found that a fluorine atom was introduced to the α-position of the nitrogen atom of N-acyl- and N-alkoxycarbonyl-2-oxazolidinones to provide the corresponding α-fluorinated products in moderate to good yields. In the case of N-phenoxycarbonyl derivative, fluorination took place on the phenyl group selectively.
Tetraethylammonium hydrogen carbonate in organic synthesis: Synthesis of oxazolidine-2,4-diones
Cesa, Stefania,Mucciante, Vittoria,Rossi, Leucio
, p. 193 - 200 (2007/10/03)
Oxazolidine-2,4-diones were synthesised by tetraethylammonium hydrogen (TEAHC) promoted carboxylation of secondary carboxamides bearing a leaving group at the α-position. Several oxazolidine-2,4-diones, including clinically used malidone, have been prepared in moderate to excellent yields as a results of a formal proton extraction-carboxylation- intramolecular S(N)2 one-pot sequence.